CYP11B2
gene geneOn this page
Also known as CYP11BLCPN2P-450C18P450aldoALDOS
Summary
CYP11B2 (cytochrome P450 family 11 subfamily B member 2, HGNC:2592) is a protein-coding gene on chromosome 8q24.3, encoding Cytochrome P450 11B2, mitochondrial (P19099). A cytochrome P450 monooxygenase that catalyzes the biosynthesis of aldosterone, the main mineralocorticoid in the human body responsible for salt and water homeostasis, thus involved in blood pressure regulation, arterial hypertension, and the development of heart failure.
This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the mitochondrial inner membrane. The enzyme has steroid 18-hydroxylase activity to synthesize aldosterone and 18-oxocortisol as well as steroid 11 beta-hydroxylase activity. Mutations in this gene cause corticosterone methyl oxidase deficiency.
Source: NCBI Gene 1585 — RefSeq curated summary.
At a glance
- Gene–disease (curated): familial hyperreninemic hypoaldosteronism type 2 (Definitive, ClinGen) — +3 more curated relationships
- GWAS associations: 16
- Clinical variants (ClinVar): 658 total — 49 pathogenic, 43 likely-pathogenic
- Phenotypes (HPO): 39
- Druggable target: yes — 12 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_000498
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:2592 |
| Approved symbol | CYP11B2 |
| Name | cytochrome P450 family 11 subfamily B member 2 |
| Location | 8q24.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CYP11BL, CPN2, P-450C18, P450aldo, ALDOS |
| Ensembl gene | ENSG00000179142 |
| Ensembl biotype | protein_coding |
| OMIM | 124080 |
| Entrez | 1585 |
Gene structure
Transcript identifiers
Ensembl transcripts: 3 — 3 protein_coding
ENST00000323110, ENST00000945895, ENST00000945896
RefSeq mRNA: 1 — MANE Select: NM_000498
NM_000498
CCDS: CCDS6393
Canonical transcript exons
ENST00000323110 — 9 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001225434 | 142912530 | 142912727 |
| ENSE00001301821 | 142917602 | 142917843 |
| ENSE00001387551 | 142910559 | 142912093 |
| ENSE00001638180 | 142914705 | 142914908 |
| ENSE00001649336 | 142915046 | 142915245 |
| ENSE00001690999 | 142912807 | 142912885 |
| ENSE00001738697 | 142917059 | 142917214 |
| ENSE00001785304 | 142913285 | 142913451 |
| ENSE00001786255 | 142914264 | 142914418 |
Expression profiles
Bgee: expression breadth broad, 30 present calls, max score 92.72.
Top tissues by expression
244 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right adrenal gland cortex | UBERON:0035827 | 92.72 | gold quality |
| right adrenal gland | UBERON:0001233 | 92.16 | gold quality |
| left adrenal gland | UBERON:0001234 | 90.22 | gold quality |
| adrenal cortex | UBERON:0001235 | 88.61 | gold quality |
| adrenal gland | UBERON:0002369 | 87.86 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 86.98 | gold quality |
| gluteal muscle | UBERON:0002000 | 84.79 | gold quality |
| parotid gland | UBERON:0001831 | 84.72 | gold quality |
| heart right ventricle | UBERON:0002080 | 83.39 | gold quality |
| triceps brachii | UBERON:0001509 | 82.10 | gold quality |
| inferior olivary complex | UBERON:0002127 | 79.43 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 78.81 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 77.28 | silver quality |
| choroid plexus epithelium | UBERON:0003911 | 76.98 | gold quality |
| olfactory bulb | UBERON:0002264 | 76.83 | gold quality |
| vena cava | UBERON:0004087 | 76.78 | gold quality |
| dorsal motor nucleus of vagus nerve | UBERON:0002870 | 76.63 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 76.35 | gold quality |
| type B pancreatic cell | CL:0000169 | 75.60 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 75.54 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 74.55 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 74.49 | gold quality |
| lateral nuclear group of thalamus | UBERON:0002736 | 73.58 | gold quality |
| cerebellar vermis | UBERON:0004720 | 73.25 | gold quality |
| body of tongue | UBERON:0011876 | 73.10 | gold quality |
| biceps brachii | UBERON:0001507 | 72.77 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 71.94 | gold quality |
| endothelial cell | CL:0000115 | 71.88 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 71.75 | gold quality |
| medulla oblongata | UBERON:0001896 | 71.50 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.98 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): APEX1, AR, ATF1, ATF2, C1QTNF1, CREB1, DMRT1, FOXL2, JUNB, NR2F1, NR4A1, NR4A2, NR5A1, REST, TCF3
miRNA regulators (miRDB)
41 targeting CYP11B2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4692 | 100.00 | 67.32 | 2066 |
| HSA-MIR-4514 | 99.99 | 67.10 | 1870 |
| HSA-MIR-512-3P | 99.97 | 67.35 | 1049 |
| HSA-MIR-4487 | 99.96 | 64.58 | 1252 |
| HSA-MIR-4731-5P | 99.89 | 67.23 | 2537 |
| HSA-MIR-7845-5P | 99.88 | 64.88 | 771 |
| HSA-MIR-549A-3P | 99.54 | 68.17 | 825 |
| HSA-MIR-671-5P | 99.52 | 67.11 | 1277 |
| HSA-MIR-6080 | 99.43 | 69.43 | 373 |
| HSA-MIR-940 | 99.37 | 66.14 | 2064 |
| HSA-MIR-6893-5P | 99.31 | 66.25 | 2119 |
| HSA-MIR-6808-5P | 99.31 | 66.23 | 2150 |
| HSA-MIR-6731-5P | 99.28 | 67.42 | 2375 |
| HSA-MIR-8085 | 99.28 | 67.56 | 2362 |
| HSA-MIR-4505 | 99.27 | 67.81 | 2678 |
| HSA-MIR-6878-3P | 99.24 | 64.23 | 920 |
| HSA-MIR-5787 | 99.22 | 67.86 | 2628 |
| HSA-MIR-6852-5P | 99.17 | 66.69 | 2073 |
| HSA-MIR-4254 | 99.11 | 65.15 | 1315 |
| HSA-MIR-485-5P | 99.10 | 64.78 | 1889 |
| HSA-MIR-6884-5P | 99.10 | 64.50 | 1987 |
| HSA-MIR-2467-3P | 98.65 | 67.18 | 1969 |
| HSA-MIR-4700-5P | 98.63 | 67.43 | 1915 |
| HSA-MIR-4722-5P | 98.46 | 66.34 | 1611 |
| HSA-MIR-5008-5P | 98.42 | 65.87 | 1019 |
| HSA-MIR-211-3P | 98.14 | 66.77 | 1052 |
| HSA-MIR-18B-3P | 98.05 | 65.55 | 595 |
| HSA-MIR-6072 | 98.00 | 66.47 | 804 |
| HSA-MIR-6765-3P | 97.83 | 64.59 | 1165 |
| HSA-MIR-3921 | 97.81 | 67.45 | 1431 |
Literature-anchored findings (GeneRIF, showing 40)
- The unmodified mitochondrial localization signal of human CYP11B2 is functional when expressed in fission yeast, and overexpression of the gene significantly enhances steroid hydroxylase activity of CYP11B2-expressing fission yeast cells. (PMID:11841224)
- Substrate recognition and conversion are attributed to the N-terminal part of human CYP11B2. (PMID:11856349)
- role in familial hyperaldosteronism (PMID:11903322)
- Differential regulation of aldosterone synthase and 11beta-hydroxylase transcription by steroidogenic factor-1 (PMID:11932209)
- investigate the relationship of gene polymorphism of angiotension converting enzyme (ACE), aldosterone synthase (CYP11B2) with essential hypertension (EH) and left ventricular hypertrophy (LVH) in hypertensive patients (PMID:12133420)
- Expression of aldosterone synthase gene in failing human heart (PMID:12161536)
- Carotid and femoral intima-media thickness were assessed in subjects genotyped for the presence of the ACE D, aldosterone synthase -344T and alpha-adducin 460Trp alleles. (PMID:12172317)
- CaMKI is involved in angiotensin II and K(+) stimulation of CYP11B2 transcription and the capacity of the adrenal to produce aldosterone (PMID:12193581)
- Inter-individual variation of blood pressure and plasma aldosterone is affected by the interaction of C(-344)T polymorphism and ageing. (PMID:12195120)
- Variation in locus contributes to hypertension in subjects with a raised aldosterone-to-renin ratio (PMID:12213905)
- CT genotype of CYP11B2 gene may be one of factors responsible for the pathogenesis of hypertrophic cardiomyopathy HCM in a proportion of patients. (PMID:12376254)
- The study of association of CYP11B2 polymorphism with hypertension in Russian patients in Bashkorstan (PMID:12391843)
- Contrasting associations between these variants and essential hypertension do not necessarily exclude the possibility that other, as yet undefined, variants of the aldosterone synthase gene could be linked with hypertension in black people. (PMID:12544440)
- Genetic variation in or near the CYP11B2 gene is a possible genetic marker for the progression of renal dysfunction in females with IgA nephropathy, but not in males (PMID:12746403)
- Linear modeling of postural changes in renin and aldosterone showed a maximal achievable aldosterone increase of 110 pmol/liter with no mutated haplotype and 500 pmol/liter with two mutated haplotypes. Molecular basis for aldosterone production. (PMID:12788845)
- Exon 3 mutation (C554T, leading to amino acid T185I) and exon 9 mutation (A1492G, leading to T498A)localize to beta 3-sheet in cytochrome P450 enzyme structure. Aldosterone synthase catalyzes oxygenation of the C(18) carbon of steroid substrates. (PMID:12788848)
- The T-344C and A6547G, but not the T4986C, variants of the aldosterone synthase gene are associated with HT in females of the Anglo-Celtic population studied. (PMID:12817181)
- A variant within the CYP11B2 locus has a clinically important impact on the severity of SBP changes in individuals with newly diagnosed hypertension who are of African ethnicity. (PMID:14643573)
- Our data suggest that -344C/T polymorphism in the promoter region of the aldosterone synthase gene affects left ventricular mass and thickness in essential hypertension, independent of adrenal aldosterone. (PMID:14736447)
- -344C/T polymorphism in CYP11B2 was considered an independent genetic factor possibly associated with hypertension or atherosclerotic diseases in the Japanese population. (PMID:15055249)
- identified two new variants in CYP11B2, a C/T single nucleotide exchange located in the first intron and a double nucleotide exchange at the 3’-splice site of exon 8 (PMID:15062555)
- The ACE I/D, alpha-adducin Gly460Trp and aldosterone synthase -344C/T polymorphisms interact to influence systolic blood pressure in Chinese, suggesting that these genes might indeed predispose to hypertension (PMID:15097233)
- Aldosterone synthase genotype is unrelated to overall coronary artery disease events risk in male patients. (PMID:15135254)
- TT genotype of T-344C polymorphism of aldosterone synthase gene was associated with significantly higher levels of plasma renin in normotensive men (PMID:15223724)
- CYP11B2 C-344T and AT1R A1166C polymorphisms affect the autonomic modulation of heart rate, but these genetic effects depend on sodium excretion. (PMID:15238568)
- In multi-ethnic population, C-344T CYP1B2 polymorphism is associated with blood pressure, plasma aldosterone levels and aldosterone-to-renin ratio. Significant differences in allele frequencies between groups. Ethnicity does not explain results. (PMID:15361760)
- Renal function in relation to ALDOS was studied in a Han population. (PMID:15378162)
- The results suggest that -344T/C polymorphism of CYP11B2 gene may be associated with low-renin essential hypertension in the Han nationality in Shandong province. (PMID:15505931)
- Molecular variant in CYP11B2 is in linkage disequilibrium (LD) with a key quantitative trait in CYP11B1. (PMID:15507509)
- Linkage disequilibrium between causative CYP11B1 variants and CYP11B2 polymorphisms account for urinary 11-deoxycortisol excretion. (PMID:15522937)
- may be polymorphic among mult=ethnic groups as a risk factor for hypertension (PMID:15545843)
- Aldo deficiency due to a compromised methyl oxidase step of Aldo synthesis favors extracellular volume depletion, and may account for an increased risk of placental hypoperfusion and consecutive development of preeclampsia (PMID:15569322)
- data support a physiological role of Ubc9 and PIAS1 as transcriptional coactivators in COUP-TFI-mediated CYP11B2 transcription (PMID:15611122)
- The CYP11B2 C-344T polymorphism affects arterial stiffness. However, sodium intake seems to modulate this genetic effect. (PMID:15614025)
- The correlation of the intron-2 conversion allele with high systolic blood pressure and plasma renin ratio associates it with hypertension. (PMID:15643128)
- Inactivating mutations cause aldosterone synthase deficiency. (PMID:15699546)
- The -344CC or intron 2 conversion (-/-) genotype in CYP11B2 may be a risk factor for developing sodium-sensitive cardiac hypertrophy. (PMID:15894890)
- aldosterone synthase gene polymorphism (ASGP) CYP11B2 influences the age-related changes in blood pressure (BP) and arterial stiffness in hypertensive subjects (PMID:15894891)
- Subjects with the combination of ACE DD and CYP11B2 CC genotypes might have a better blood pressure response to hydrochlorothiazide than the other genotypic combinations of these 2 genes. (PMID:16080804)
- The CYP11B-344C/T polymorphism is associated with small artery compliance, and TT genotype subjects are susceptible to abnormality of small arterial compliance. (PMID:16080805)
Cross-species orthologs
0 orthologs
Paralogs (2): CYP11A1 (ENSG00000140459), CYP11B1 (ENSG00000160882)
Protein
Protein identifiers
Cytochrome P450 11B2, mitochondrial — P19099 (reviewed: P19099)
Alternative names: Aldosterone synthase, Aldosterone-synthesizing enzyme, CYPXIB2, Corticosterone 18-monooxygenase, CYP11B2, Cytochrome P-450Aldo, Cytochrome P-450C18, Steroid 11-beta-hydroxylase, CYP11B2, Steroid 18-hydroxylase
All UniProt accessions (1): P19099
UniProt curated annotations — full annotation on UniProt →
Function. A cytochrome P450 monooxygenase that catalyzes the biosynthesis of aldosterone, the main mineralocorticoid in the human body responsible for salt and water homeostasis, thus involved in blood pressure regulation, arterial hypertension, and the development of heart failure. Catalyzes three sequential oxidative reactions of 11-deoxycorticosterone (21-hydroxyprogesterone), namely 11-beta hydroxylation, followed by two successive oxidations at C18 yielding 18-hydroxy and then 18-oxo intermediates (that would not leave the enzyme active site during the consecutive hydroxylation reactions), ending with the formation of aldosterone. Can also produce 18-hydroxycortisol and 18-oxocortisol, derived from successive oxidations of cortisol at C18, normally found at very low levels, but significantly increased in primary aldosteronism, the most common form of secondary hypertension. Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate and reducing the second into a water molecule. Two electrons are provided by NADPH via a two-protein mitochondrial transfer system comprising flavoprotein FDXR (adrenodoxin/ferredoxin reductase) and nonheme iron-sulfur protein FDX1 or FDX2 (adrenodoxin/ferredoxin). Could also be involved in the androgen metabolic pathway.
Subcellular location. Mitochondrion inner membrane.
Tissue specificity. Expressed sporadically in the zona glomerulosa (zG) of the adrenal cortex (conventional zonation), as well as in aldosterone-producing cell clusters (APCCs) composed of morphological zG cells in contact with the capsule (variegated zonation).
Disease relevance. Corticosterone methyloxidase 1 deficiency (CMO-1 deficiency) [MIM:203400] Autosomal recessive disorder of aldosterone biosynthesis. There are two biochemically different forms of selective aldosterone deficiency be termed corticosterone methyloxidase (CMO) deficiency type 1 and type 2. In CMO-1 deficiency, aldosterone is undetectable in plasma, while its immediate precursor, 18-hydroxycorticosterone, is low or normal. The disease is caused by variants affecting the gene represented in this entry. Corticosterone methyloxidase 2 deficiency (CMO-2 deficiency) [MIM:610600] Autosomal recessive disorder of aldosterone biosynthesis. In CMO-2 deficiency, aldosterone can be low or normal, but at the expense of increased secretion of 18-hydroxycorticosterone. Consequently, patients have a greatly increased ratio of 18-hydroxycorticosterone to aldosterone and a low ratio of corticosterone to 18-hydroxycorticosterone in serum. The disease is caused by variants affecting the gene represented in this entry.
Induction. Expression is induced by angiotensin II, potassium (K+), and also by cAMP.
Pathway. Steroid biosynthesis.
Miscellaneous. Expressed in aldosterone-secreting tumors and in adrenal glands of patients with idiopathic hyperaldosteronism.
Similarity. Belongs to the cytochrome P450 family.
RefSeq proteins (1): NP_000489* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001128 | Cyt_P450 | Family |
| IPR002399 | Cyt_P450_mitochondrial | Family |
| IPR017972 | Cyt_P450_CS | Conserved_site |
| IPR036396 | Cyt_P450_sf | Homologous_superfamily |
| IPR050479 | CYP11_CYP27_families | Family |
Pfam: PF00067
Enzyme classification (BRENDA):
- EC 1.14.15.4 — steroid 11beta-monooxygenase (BRENDA: 16 organisms, 122 substrates, 309 inhibitors, 38 Km, 19 kcat entries)
- EC 1.14.15.5 — corticosterone 18-monooxygenase (BRENDA: 5 organisms, 15 substrates, 98 inhibitors, 3 Km, 1 kcat entries)
Substrate kinetics (BRENDA)
7 substrates with measured Km, best-characterized 7. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| 11-DEOXYCORTICOSTERONE | 0.0008–0.18 | 15 |
| 11-DEOXYCORTISOL | 0.0084–0.338 | 6 |
| CORTICOSTERONE | 0.0059–0.087 | 4 |
| ADRENAL FERREDOXIN | 0.002–0.0024 | 2 |
| DEOXYCORTICOSTERONE | 0.006–0.02 | 2 |
| 4-ANDROSTENE-3,17-DIONE | 0.013 | 1 |
| CORTICOSTERONE | 0.028 | 1 |
Catalyzed reactions (Rhea), 8 shown:
- corticosterone + 2 reduced [adrenodoxin] + O2 + 2 H(+) = 18-hydroxycorticosterone + 2 oxidized [adrenodoxin] + H2O (RHEA:11872)
- a steroid + 2 reduced [adrenodoxin] + O2 + 2 H(+) = an 11beta-hydroxysteroid + 2 oxidized [adrenodoxin] + H2O (RHEA:15629)
- 11-deoxycortisol + 2 reduced [adrenodoxin] + O2 + 2 H(+) = cortisol + 2 oxidized [adrenodoxin] + H2O (RHEA:46100)
- 21-hydroxyprogesterone + 2 reduced [adrenodoxin] + O2 + 2 H(+) = corticosterone + 2 oxidized [adrenodoxin] + H2O (RHEA:46104)
- 18-hydroxycorticosterone + 2 reduced [adrenodoxin] + O2 + 2 H(+) = aldosterone + 2 oxidized [adrenodoxin] + 2 H2O (RHEA:50792)
- cortisol + 2 reduced [adrenodoxin] + O2 + 2 H(+) = 18-hydroxycortisol + 2 oxidized [adrenodoxin] + H2O (RHEA:76019)
- 18-hydroxycortisol + 2 reduced [adrenodoxin] + O2 + 2 H(+) = 18-oxocortisol + 2 oxidized [adrenodoxin] + 2 H2O (RHEA:76023)
- 21-hydroxyprogesterone + 2 reduced [adrenodoxin] + O2 + 2 H(+) = 18-hydroxy-11-deoxycorticosterone + 2 oxidized [adrenodoxin] + H2O (RHEA:76151)
UniProt features (70 total): helix 24, sequence variant 18, strand 13, sequence conflict 7, mutagenesis site 3, binding site 2, transit peptide 1, chain 1, turn 1
Structure
Experimental structures (PDB)
7 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 4DVQ | X-RAY DIFFRACTION | 2.49 |
| 4FDH | X-RAY DIFFRACTION | 2.71 |
| 6XZ9 | X-RAY DIFFRACTION | 2.77 |
| 7M8I | X-RAY DIFFRACTION | 2.94 |
| 6XZ8 | X-RAY DIFFRACTION | 3 |
| 7M8V | X-RAY DIFFRACTION | 3.08 |
| 4ZGX | X-RAY DIFFRACTION | 3.2 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P19099-F1 | 90.10 | 0.74 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (2): 381; 450 (axial binding residue)
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 112 | increases 11-beta- and 18-hydroxylase activities toward 11-deoxycorticosterone; increases 11-beta-hydroxylase activity t |
| 147 | increases 11-beta-hydroxylase activity toward 11-deoxycorticosterone and 11-deoxycortisol. |
| 152 | no significant effect on hydroxylase activities toward 11-deoxycorticosterone and 11-deoxycortisol. |
Function
Pathways and Gene Ontology
Reactome pathways
14 pathways
| ID | Pathway |
|---|---|
| R-HSA-193993 | Mineralocorticoid biosynthesis |
| R-HSA-194002 | Glucocorticoid biosynthesis |
| R-HSA-211976 | Endogenous sterols |
| R-HSA-5579009 | Defective CYP11B2 causes CMO-1 deficiency |
| R-HSA-1430728 | Metabolism |
| R-HSA-1643685 | Disease |
| R-HSA-196071 | Metabolism of steroid hormones |
| R-HSA-211859 | Biological oxidations |
| R-HSA-211897 | Cytochrome P450 - arranged by substrate type |
| R-HSA-211945 | Phase I - Functionalization of compounds |
| R-HSA-556833 | Metabolism of lipids |
| R-HSA-5579029 | Metabolic disorders of biological oxidation enzymes |
| R-HSA-5668914 | Diseases of metabolism |
| R-HSA-8957322 | Metabolism of steroids |
MSigDB gene sets: 309 (showing top):
MODULE_93, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, REACTOME_BIOLOGICAL_OXIDATIONS, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_PAIRED_DONORS_WITH_INCORPORATION_OR_REDUCTION_OF_MOLECULAR_OXYGEN, GNF2_GSTM1, PEREZ_TP63_TARGETS, GOBP_GLUCOCORTICOID_METABOLIC_PROCESS, GOBP_RENAL_SYSTEM_PROCESS_INVOLVED_IN_REGULATION_OF_BLOOD_VOLUME, GNF2_HPN, GOBP_C21_STEROID_HORMONE_METABOLIC_PROCESS, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE, GOBP_REGULATION_OF_HORMONE_LEVELS
GO Biological Process (19): regulation of blood volume by renal aldosterone (GO:0002017), renal water homeostasis (GO:0003091), C21-steroid hormone biosynthetic process (GO:0006700), glucocorticoid biosynthetic process (GO:0006704), mineralocorticoid biosynthetic process (GO:0006705), cholesterol metabolic process (GO:0008203), sterol metabolic process (GO:0016125), aldosterone biosynthetic process (GO:0032342), cellular response to hormone stimulus (GO:0032870), cortisol metabolic process (GO:0034650), cortisol biosynthetic process (GO:0034651), cellular response to potassium ion (GO:0035865), potassium ion homeostasis (GO:0055075), sodium ion homeostasis (GO:0055078), cellular response to peptide hormone stimulus (GO:0071375), alcohol metabolic process (GO:0006066), lipid metabolic process (GO:0006629), steroid biosynthetic process (GO:0006694), steroid metabolic process (GO:0008202)
GO Molecular Function (9): steroid 11-beta-monooxygenase activity (GO:0004507), iron ion binding (GO:0005506), steroid hydroxylase activity (GO:0008395), heme binding (GO:0020037), corticosterone 18-monooxygenase activity (GO:0047783), monooxygenase activity (GO:0004497), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen (GO:0016705), metal ion binding (GO:0046872)
GO Cellular Component (3): mitochondrion (GO:0005739), mitochondrial inner membrane (GO:0005743), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-10 pathways:
| Category | Pathways |
|---|---|
| Metabolism of steroid hormones | 2 |
| Metabolism | 2 |
| Cytochrome P450 - arranged by substrate type | 1 |
| Metabolic disorders of biological oxidation enzymes | 1 |
| Metabolism of steroids | 1 |
| Phase I - Functionalization of compounds | 1 |
| Biological oxidations | 1 |
| Diseases of metabolism | 1 |
| Disease | 1 |
| Metabolism of lipids | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| steroid hormone biosynthetic process | 3 |
| hormone biosynthetic process | 2 |
| glucocorticoid metabolic process | 2 |
| steroid metabolic process | 2 |
| primary alcohol biosynthetic process | 2 |
| ketone biosynthetic process | 2 |
| olefinic compound biosynthetic process | 2 |
| monoatomic cation homeostasis | 2 |
| inorganic ion homeostasis | 2 |
| oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced iron-sulfur protein as one donor, and incorporation of one atom of oxygen | 2 |
| oxidoreductase activity | 2 |
| regulation of systemic arterial blood pressure by hormone | 1 |
| positive regulation of systemic arterial blood pressure | 1 |
| renal system process | 1 |
| multicellular organismal-level water homeostasis | 1 |
| C21-steroid hormone metabolic process | 1 |
| mineralocorticoid metabolic process | 1 |
| sterol metabolic process | 1 |
| secondary alcohol metabolic process | 1 |
| C21-steroid hormone biosynthetic process | 1 |
| mineralocorticoid biosynthetic process | 1 |
| aldosterone metabolic process | 1 |
| aldehyde biosynthetic process | 1 |
| response to hormone | 1 |
| cellular response to chemical stimulus | 1 |
| cellular response to endogenous stimulus | 1 |
| primary alcohol metabolic process | 1 |
| ketone metabolic process | 1 |
| olefinic compound metabolic process | 1 |
| tertiary alcohol metabolic process | 1 |
| glucocorticoid biosynthetic process | 1 |
| cortisol metabolic process | 1 |
| tertiary alcohol biosynthetic process | 1 |
| response to potassium ion | 1 |
| cellular response to metal ion | 1 |
| cellular response to hormone stimulus | 1 |
| response to peptide hormone | 1 |
| cellular response to nitrogen compound | 1 |
| cellular response to oxygen-containing compound | 1 |
| small molecule metabolic process | 1 |
Protein interactions and networks
STRING
1708 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CYP11B2 | STAR | P49675 | 922 |
| CYP11B2 | REN | P00797 | 912 |
| CYP11B2 | HSD11B2 | P80365 | 901 |
| CYP11B2 | AGT | P01019 | 897 |
| CYP11B2 | AGTR1 | P30556 | 871 |
| CYP11B2 | ACE | P12821 | 864 |
| CYP11B2 | MC2R | Q01718 | 842 |
| CYP11B2 | NR5A1 | Q13285 | 829 |
| CYP11B2 | POMC | P01189 | 818 |
| CYP11B2 | FDX1 | P10109 | 812 |
| CYP11B2 | KCNJ5 | P48544 | 812 |
| CYP11B2 | HSD3B2 | P26439 | 794 |
| CYP11B2 | NR3C2 | P08235 | 792 |
| CYP11B2 | ATP2B3 | Q16720 | 763 |
| CYP11B2 | NR0B1 | P51843 | 757 |
IntAct
0 interactions, top by confidence:
BioGRID (10): CYP11B2 (Negative Genetic), HMGA1 (Negative Genetic), SSTR5 (Negative Genetic), MAP3K10 (Negative Genetic), PIM1 (Negative Genetic), CYP11B2 (Negative Genetic), CYP11B2 (Affinity Capture-MS), CYP11B2 (Affinity Capture-Western), TRIM2 (Affinity Capture-Western), CYP11B2 (Co-crystal Structure)
ESM2 similar proteins: O15528, O35074, O46515, O77809, O77810, P00187, P00189, P05108, P05177, P10611, P10612, P14137, P14579, P14580, P14581, P15150, P15393, P15538, P15539, P17177, P17178, P19099, P30099, P30100, P51663, P79153, P79202, P97720, Q02318, Q02928, Q07217, Q16647, Q28827, Q29527, Q29552, Q29626, Q2XV99, Q4H4C3, Q5KQT6, Q5TCH4
Diamond homologs: A0A068Q5V6, A0A068Q605, A0A068Q7V0, A0A0C5QRZ2, A0A0D9MRV9, A0A0N7F297, A0A1B4XBH0, A0A1B4XBH8, A0A1D6F9Y9, A0A1D6HSP4, A0A1W5T1Y6, A0A2H5AIX6, A0A2K9RG08, A0A3Q9R4N5, A0A4D6Q414, A0A4D6Q415, A0A517FNC5, A0A8K1AW54, A2QBE8, A6YIH8, B1GVX3, B8NHD9, B8NHY4, C9K202, D1MX85, E9KMQ3, E9Q816, F2K081, F4JW83, G3XSI3, G4N2X2, G5EJN7, H2DH18, H2DH24, L0N063, L7HT17, M1KVN4, M1KXD0, O13345, O22203
SIGNOR signaling
9 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| APEX1 | “down-regulates quantity by repression” | CYP11B2 | “transcriptional regulation” |
| NR5A1 | “down-regulates quantity by repression” | CYP11B2 | “transcriptional regulation” |
| CYP11B2 | “up-regulates quantity” | cortisol | “chemical modification” |
| CYP11B2 | “down-regulates quantity” | 11-deoxycortisol | “chemical modification” |
| CYP11B2 | “up-regulates quantity” | corticosterone | “chemical modification” |
| CYP11B2 | “down-regulates quantity” | 11-deoxycorticosterone | “chemical modification” |
| CYP11B2 | “up-regulates quantity” | 18-hydroxycorticosterone | “chemical modification” |
| CYP11B2 | “up-regulates quantity” | aldosterone | “chemical modification” |
| metyrapone | “down-regulates activity” | CYP11B2 | “chemical inhibition” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
658 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 49 |
| Likely pathogenic | 43 |
| Uncertain significance | 162 |
| Likely benign | 334 |
| Benign | 24 |
Top pathogenic / likely-pathogenic (30)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1071836 | NM_000498.3(CYP11B2):c.342_343dup (p.Pro115fs) | Pathogenic |
| 1073733 | NM_000498.3(CYP11B2):c.1276C>T (p.Gln426Ter) | Pathogenic |
| 1074429 | NC_000008.10:g.(?143998465)(143999600_?)del | Pathogenic |
| 1374879 | NM_000498.3(CYP11B2):c.553del (p.Thr185fs) | Pathogenic |
| 1387027 | NM_000498.3(CYP11B2):c.595+1del | Pathogenic |
| 1414779 | NM_000498.3(CYP11B2):c.1034_1047del (p.Leu345fs) | Pathogenic |
| 1416764 | NM_000498.3(CYP11B2):c.1066C>T (p.Gln356Ter) | Pathogenic |
| 1455200 | NM_000498.3(CYP11B2):c.531del (p.Gln178fs) | Pathogenic |
| 1458193 | NM_000498.3(CYP11B2):c.892G>T (p.Glu298Ter) | Pathogenic |
| 1459295 | NM_000498.3(CYP11B2):c.217C>T (p.Gln73Ter) | Pathogenic |
| 16878 | NM_000498.3(CYP11B2):c.104_109delinsG (p.Val35fs) | Pathogenic |
| 16881 | NM_000498.3(CYP11B2):c.554C>T (p.Thr185Ile) | Pathogenic |
| 16884 | CYP11B2, IVS2 CONVERSION | Pathogenic |
| 2027037 | NM_000498.3(CYP11B2):c.916dup (p.Ala306fs) | Pathogenic |
| 2031382 | NM_000498.3(CYP11B2):c.845del (p.Arg282fs) | Pathogenic |
| 2097019 | NM_000498.3(CYP11B2):c.1084del (p.Leu362fs) | Pathogenic |
| 2098081 | NM_000498.3(CYP11B2):c.895del (p.Leu299fs) | Pathogenic |
| 2109017 | NM_000498.3(CYP11B2):c.240-1G>T | Pathogenic |
| 2119763 | NM_000498.3(CYP11B2):c.1247T>A (p.Leu416Ter) | Pathogenic |
| 2136711 | NM_000498.3(CYP11B2):c.788T>A (p.Ile263Asn) | Pathogenic |
| 2136713 | NM_000498.3(CYP11B2):c.508C>T (p.Gln170Ter) | Pathogenic |
| 2423179 | NC_000008.10:g.(?143993936)(143994311_?)del | Pathogenic |
| 2674683 | NM_000498.3(CYP11B2):c.546dup (p.Ser183fs) | Pathogenic |
| 2674686 | NM_000498.3(CYP11B2):c.793C>T (p.Gln265Ter) | Pathogenic |
| 2674688 | NM_000498.3(CYP11B2):c.954G>C (p.Thr318=) | Pathogenic |
| 2674696 | NM_000498.3(CYP11B2):c.1471C>T (p.Pro491Ser) | Pathogenic |
| 2697591 | NM_000498.3(CYP11B2):c.594A>T (p.Glu198Asp) | Pathogenic |
| 2702769 | NM_000498.3(CYP11B2):c.499del (p.Asp167fs) | Pathogenic |
| 2703927 | NM_000498.3(CYP11B2):c.1140del (p.Leu382fs) | Pathogenic |
| 2704824 | NM_000498.3(CYP11B2):c.180_184del (p.Tyr61fs) | Pathogenic |
SpliceAI
1591 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 8:142912528:A:AC | donor_gain | 1.0000 |
| 8:142912529:C:CC | donor_gain | 1.0000 |
| 8:142914276:C:CA | donor_gain | 1.0000 |
| 8:142914416:CAC:C | acceptor_gain | 1.0000 |
| 8:142914419:C:CC | acceptor_gain | 1.0000 |
| 8:142914419:CT:C | acceptor_loss | 1.0000 |
| 8:142914424:C:CT | acceptor_gain | 1.0000 |
| 8:142914424:C:T | acceptor_gain | 1.0000 |
| 8:142914704:CCGTA:C | donor_gain | 1.0000 |
| 8:142914708:A:AC | donor_gain | 1.0000 |
| 8:142914709:C:CC | donor_gain | 1.0000 |
| 8:142915041:CACA:C | donor_loss | 1.0000 |
| 8:142915042:ACAC:A | donor_loss | 1.0000 |
| 8:142915044:ACC:A | donor_loss | 1.0000 |
| 8:142915045:C:A | donor_loss | 1.0000 |
| 8:142915045:CCTT:C | donor_gain | 1.0000 |
| 8:142915081:T:TA | donor_gain | 1.0000 |
| 8:142915241:CATTC:C | acceptor_gain | 1.0000 |
| 8:142915242:ATTC:A | acceptor_gain | 1.0000 |
| 8:142915243:TTC:T | acceptor_gain | 1.0000 |
| 8:142915243:TTCC:T | acceptor_loss | 1.0000 |
| 8:142915244:TC:T | acceptor_gain | 1.0000 |
| 8:142915245:CC:C | acceptor_gain | 1.0000 |
| 8:142915246:C:CA | acceptor_loss | 1.0000 |
| 8:142915246:C:CC | acceptor_gain | 1.0000 |
| 8:142915247:T:G | acceptor_loss | 1.0000 |
| 8:142917057:A:AC | donor_gain | 1.0000 |
| 8:142917058:C:CC | donor_gain | 1.0000 |
| 8:142917058:CAA:C | donor_gain | 1.0000 |
| 8:142917123:T:TA | donor_gain | 1.0000 |
AlphaMissense
3288 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 8:142912599:A:C | F443L | 0.993 |
| 8:142912599:A:T | F443L | 0.993 |
| 8:142912601:A:G | F443L | 0.993 |
| 8:142914904:G:C | S200R | 0.990 |
| 8:142914904:G:T | S200R | 0.990 |
| 8:142914906:T:G | S200R | 0.990 |
| 8:142915230:C:A | W137C | 0.990 |
| 8:142915230:C:G | W137C | 0.990 |
| 8:142915232:A:G | W137R | 0.990 |
| 8:142915232:A:T | W137R | 0.990 |
| 8:142914273:G:C | S315R | 0.989 |
| 8:142914273:G:T | S315R | 0.989 |
| 8:142914275:T:G | S315R | 0.989 |
| 8:142913374:G:C | S344R | 0.987 |
| 8:142913374:G:T | S344R | 0.987 |
| 8:142913376:T:G | S344R | 0.987 |
| 8:142913294:T:A | E371V | 0.985 |
| 8:142915219:C:G | R141P | 0.985 |
| 8:142912578:G:C | C450W | 0.984 |
| 8:142917108:A:G | W116R | 0.984 |
| 8:142917108:A:T | W116R | 0.984 |
| 8:142914726:A:G | W260R | 0.982 |
| 8:142914726:A:T | W260R | 0.982 |
| 8:142911996:A:G | F499S | 0.981 |
| 8:142912570:C:G | R453P | 0.981 |
| 8:142912580:A:G | C450R | 0.981 |
| 8:142914286:A:G | L311P | 0.981 |
| 8:142912586:G:T | R448S | 0.979 |
| 8:142913295:C:T | E371K | 0.978 |
| 8:142913414:G:T | A331D | 0.978 |
dbSNP variants (sampled 300 via entrez): RS1000182985 (8:142919583 TTTA>T), RS1000921788 (8:142913188 G>A), RS1001157479 (8:142913564 A>C), RS1001183450 (8:142918518 C>T), RS1002584292 (8:142916815 C>T), RS1002643099 (8:142916630 C>G,T), RS1002764645 (8:142911426 G>A,C,T), RS1002935857 (8:142911207 A>G), RS1003528368 (8:142919753 A>G), RS1004313400 (8:142918871 C>T), RS1005277521 (8:142910633 C>A,T), RS1005726427 (8:142912320 C>G,T), RS1005931936 (8:142916389 C>A,G), RS1006012671 (8:142911126 A>G), RS1006065351 (8:142910921 G>A)
Disease associations
OMIM: gene MIM:124080 | disease phenotypes: MIM:203400, MIM:610600, MIM:103900, MIM:606984
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| corticosterone methyloxidase type 2 deficiency | Strong | Autosomal recessive |
| corticosterone methyloxidase type 1 deficiency | Moderate | Autosomal recessive |
| familial hypoaldosteronism | Supportive | Autosomal recessive |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| familial hyperreninemic hypoaldosteronism type 2 | Definitive | AR |
Mondo (6): corticosterone methyloxidase type 1 deficiency (MONDO:0008751), corticosterone methyloxidase type 2 deficiency (MONDO:0012524), glucocorticoid-remediable aldosteronism (MONDO:0007080), early-onset familial hypoaldosteronism (MONDO:0035320), familial hypoaldosteronism (MONDO:0018541), familial hyperreninemic hypoaldosteronism type 2 (MONDO:0011754)
Orphanet (4): Familial hypoaldosteronism (Orphanet:427), Familial hyperaldosteronism type I (Orphanet:403), Early-onset familial hypoaldosteronism (Orphanet:556030), OBSOLETE: Familial hyperreninemic hypoaldosteronism type 2 (Orphanet:99764)
HPO phenotypes
39 total (30 of 39 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000007 | Autosomal recessive inheritance |
| HP:0000127 | Renal salt wasting |
| HP:0000360 | Tinnitus |
| HP:0000421 | Epistaxis |
| HP:0000811 | Abnormal external genitalia morphology |
| HP:0000822 | Hypertension |
| HP:0000848 | Increased circulating renin concentration |
| HP:0001278 | Orthostatic hypotension |
| HP:0001290 | Generalized hypotonia |
| HP:0001324 | Muscle weakness |
| HP:0001508 | Failure to thrive |
| HP:0001510 | Growth delay |
| HP:0001944 | Dehydration |
| HP:0001954 | Recurrent fever |
| HP:0001959 | Polydipsia |
| HP:0002013 | Vomiting |
| HP:0002018 | Nausea |
| HP:0002153 | Hyperkalemia |
| HP:0002170 | Intracranial hemorrhage |
| HP:0002315 | Headache |
| HP:0002615 | Hypotension |
| HP:0002900 | Hypokalemia |
| HP:0002902 | Hyponatremia |
| HP:0003623 | Neonatal onset |
| HP:0004319 | Decreased circulating aldosterone concentration |
| HP:0008221 | Adrenal hyperplasia |
| HP:0008872 | Feeding difficulties in infancy |
| HP:0008897 | Postnatal growth retardation |
| HP:0011410 | Caesarean section |
| HP:0011739 | Dexamethasone-suppressible primary hyperaldosteronism |
GWAS associations
16 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004363_4 | Plasma androstenedione levels in resected early stage-receptor positive breast cancer | 7.000000e-07 |
| GCST005979_15 | Systolic blood pressure | 4.000000e-12 |
| GCST006010_12 | Mean arterial pressure | 9.000000e-11 |
| GCST007094_188 | Diastolic blood pressure | 6.000000e-10 |
| GCST007095_90 | Systolic blood pressure | 8.000000e-06 |
| GCST007099_199 | Systolic blood pressure | 3.000000e-10 |
| GCST007267_336 | Systolic blood pressure | 1.000000e-10 |
| GCST007703_109 | Systolic blood pressure | 1.000000e-11 |
| GCST007704_19 | Diastolic blood pressure | 3.000000e-09 |
| GCST007705_1 | Pulse pressure | 7.000000e-06 |
| GCST007706_31 | Mean arterial pressure | 1.000000e-11 |
| GCST007706_54 | Mean arterial pressure | 1.000000e-11 |
| GCST007707_31 | Hypertension | 2.000000e-08 |
| GCST007707_60 | Hypertension | 3.000000e-08 |
| GCST007928_81 | Medication use (diuretics) | 3.000000e-09 |
| GCST011141_21 | Hypertension | 3.000000e-08 |
EFO canonical traits (6, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007972 | androstenedione measurement |
| EFO:0006335 | systolic blood pressure |
| EFO:0006340 | mean arterial pressure |
| EFO:0006336 | diastolic blood pressure |
| EFO:0005763 | pulse pressure measurement |
| EFO:0009928 | Diuretic use measurement |
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| C563177 | Glucocorticoid-Remediable Aldosteronism (supp.) | |
| C564638 | Hyperreninemic Hypoaldosteronism, Familial, 2 (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2722 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
12 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 281,966 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL106 | FLUCONAZOLE | 4 | 58,942 |
| CHEMBL1397 | POSACONAZOLE | 4 | 541 |
| CHEMBL1444 | LETROZOLE | 4 | 81,122 |
| CHEMBL157101 | KETOCONAZOLE | 4 | 75,361 |
| CHEMBL254328 | ABIRATERONE | 4 | 22,316 |
| CHEMBL3099695 | OSILODROSTAT | 4 | 347 |
| CHEMBL681 | ETOMIDATE | 4 | 8,462 |
| CHEMBL934 | METYRAPONE | 4 | 2,893 |
| CHEMBL4113975 | BAXDROSTAT | 3 | 16 |
| CHEMBL5095105 | LORUNDROSTAT | 3 | 35 |
| CHEMBL287677 | DEXFADROSTAT | 2 | 169 |
| CHEMBL9298 | FADROZOLE | 2 | 31,762 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
2 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs1799998 | Efficacy | 3 | benazepril;imidapril | Essential hypertension |
| rs1799998 | Efficacy | 3 | candesartan | Hypertension |
PharmGKB variants
1 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs1799998 | CYP11B2 | 3 | 2.50 | 2 | benazepril;imidapril;candesartan |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — CYP11, CYP17, CYP19, CYP20 and CYP21 families
Most potent curated ligand interactions (7 total), top 7:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| osilodrostat | Inhibition | 9.7 | pIC50 |
| fadrozole | Inhibition | 9.1 | pKi |
| lorundrostat | Inhibition | 8.9 | pKi |
| dexfadrostat | Inhibition | 7.97 | pIC50 |
| baxdrostat | Inhibition | 7.89 | pKi |
| vicadrostat | Inhibition | 7.8 | pIC50 |
| metyrapone | Inhibition | 7.1 | pIC50 |
Binding affinities (BindingDB)
1017 measured of 1102 human assays (1102 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| (E)-2-(4-Chlorophenoxy)-3- (dimethylamino)-1-(2-methoxyphenyl)prop- 2-en-1-one | EC50 | 0.001 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[(Z)-1-(2-Benzyloxybenzoyl)-2- (dimethylamino)vinyloxy]benzonitrile | EC50 | 0.001 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00174 | EC50 | 0.003 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00182 | EC50 | 0.005 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-[2-(Pyridin-4-ylmethoxy)phenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.007 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00175 | EC50 | 0.007 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00172 | EC50 | 0.011 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00173 | EC50 | 0.011 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-(2-Fluoro-3-hydroxyphenyl)-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.017 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (E)-1-[(2-Chlorobenzoyl)-2- (dimethylamino)vinyloxy]benzonitrile | EC50 | 0.018 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00183 | EC50 | 0.028 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| Methyl 3-[(E)-2-(4-cyanophenoxy)- 3-(dimethylamino)prop-2-enoyl]benzoate | EC50 | 0.031 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00129 | EC50 | 0.032 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-[3-[[3-Fluoro-3-(hydroxymethyl)azetidin-1-yl]methyl]phenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.036 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00162 | EC50 | 0.038 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00131 | EC50 | 0.046 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-[3-[(6-Fluoropyridin-2-yl)oxymethyl]phenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.048 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (rac)-6-[4-[1-(1-Acetylpiperidin-4-yl)ethyl]-1H-pyrazol-3-yl]-5-fluoro-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.049 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| 4-[3-[3-(pyridin-3-ylmethoxy)phenyl]pyrazolidin-4-yl]oxybenzonitrile | EC50 | 0.051 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (E)-2-(4-Chlorophenoxy)-1-(2- chlorophenyl)-3-(dimethylamino)prop-2-en- 1-one | EC50 | 0.052 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-[3-(Pyridin-2-ylmethoxy)phenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.052 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[(Z)-1-(3-Benzyloxybenzoyl)-2- (dimethylamino)vinyloxy]benzonitrile | EC50 | 0.053 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (rac)-6-[4-[1-(1-Acetylpiperidin-4-yl)ethyl]-1H-pyrazol-3-yl]-7-fluoro-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.067 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| 4-[(Z)-1-(2-Chloro-3-fluoro- benzoyl)- (dimethylamino)vinyloxy]benzonitrile | EC50 | 0.069 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (+)-6-[4-[(1R)-1-(1-acetylpiperidin-4-yl)ethyl]-1H-pyrazol-3-yl]-5-fluoro-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.074 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| (E)-2-(4-Chlorophenoxy)-1-[2- (difluoromethoxy)phenyl]-3- (dimethylamino)prop-2-en-1-one | EC50 | 0.076 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00074 | EC50 | 0.076 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| 4-[[3-(3-Hydroxyphenyl)-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.083 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-[3-(Hydroxymethyl)phenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.085 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00133 | EC50 | 0.094 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 1-methyl-6-[5-[(6-methyl-2-pyridinyl)sulfanylmethyl]-3-pyridinyl]-3,4-dihydroquinolin-2-one | EC50 | 0.1 nM | US-9458135: Dihydroquinoline-2-one derivatives |
| 4-[[5-(3-Butoxyphenyl)-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.102 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00072 | EC50 | 0.133 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| 4-[(E)-1-(2-Chlorobenzoyl)-2- (dimethylamino)vinyloxy]-3-fluoro- benzonitrile | EC50 | 0.134 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 4-[[3-[3-(Morpholin-4-ylmethyl)phenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.139 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (rac)-4-[[3-[1-(1-Methylpyrazole-4-carbonyl)piperidin-3-yl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.15 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (E)-2-(4-Chlorophenoxy)-1-(2,4- difluorophenyl)-3-(dimethylamino)prop-2- en-1-one | EC50 | 0.159 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00117 | EC50 | 0.159 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (E)-1-[(2,3-Difluorobenzoyl)-2-(dimethylamino)vinyloxy]benzonitrile | EC50 | 0.161 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (E)-2-(4-Chlorophenoxy)-3- (dimethylamino)-1-(2-fluorophenyl)prop-2- en-1-one | EC50 | 0.167 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00176 | EC50 | 0.171 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 6-[4-[(1-Acetyl-4-piperidyl)methyl]-1H-pyrazol-3-yl]-5-fluoro-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.184 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| 4-[(E)-1-(3-Chloro-2-fluoro- benzoyl)-2- (dimethylamino)vinyloxy]benzonitrile | EC50 | 0.191 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CHEM-US-00130 | EC50 | 0.198 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (rac)-4-[[3-[3-(1-Acetylpyrrolidin-3-yl)oxyphenyl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.215 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 5-Chloro-6-[4-[(2-ethylsulfonyl-2-azaspiro[3.3]heptan-6-yl)methyl]-1H-pyrazol-3-yl]-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.215 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| 6-[4-[(1-Ethylsulfonyl-4-piperidyl)methyl]-1H-pyrazol-3-yl]-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.216 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
| (rac)-3-Fluoro-4-[[5-[1-(1-methylpyrazole-4-carbonyl)piperidin-3-yl]-1H-pyrazol-4-yl]oxy]benzonitrile | EC50 | 0.231 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| (E)-1-(2-Chloro-3-fluoro-phenyl)-2- (4-chlorophenoxy)-3-(dimethylamino)prop-2- en-1-one | EC50 | 0.262 nM | US-9790217: Pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| 6-[4-[(1-Acetyl-4-piperidyl)methyl]-1H-pyrazol-3-yl]-1-methyl-3,4-dihydroquinolin-2-one | EC50 | 0.266 nM | US-9796702: Dihydroquinoline pyrazolyl compounds |
ChEMBL bioactivities
3025 potent at pChembl≥5 of 3043 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 11.00 | EC50 | 0.01 | nM | CHEMBL5794024 |
| 11.00 | EC50 | 0.01 | nM | CHEMBL5955547 |
| 11.00 | EC50 | 0.01 | nM | CHEMBL6056586 |
| 11.00 | EC50 | 0.01 | nM | CHEMBL5993024 |
| 11.00 | EC50 | 0.01 | nM | CHEMBL5806425 |
| 10.96 | EC50 | 0.011 | nM | CHEMBL5846526 |
| 10.96 | EC50 | 0.011 | nM | CHEMBL5754409 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL3916961 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL5849911 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL5767596 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL5877749 |
| 10.89 | EC50 | 0.013 | nM | CHEMBL5789906 |
| 10.85 | EC50 | 0.014 | nM | CHEMBL4632981 |
| 10.85 | EC50 | 0.014 | nM | CHEMBL5960934 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL5935291 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL5901252 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL5965994 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL5870745 |
| 10.80 | EC50 | 0.016 | nM | CHEMBL5760532 |
| 10.77 | EC50 | 0.017 | nM | CHEMBL5928932 |
| 10.77 | EC50 | 0.017 | nM | CHEMBL5949511 |
| 10.77 | EC50 | 0.017 | nM | CHEMBL5848123 |
| 10.74 | EC50 | 0.018 | nM | CHEMBL5965425 |
| 10.74 | EC50 | 0.018 | nM | CHEMBL6020579 |
| 10.72 | EC50 | 0.019 | nM | CHEMBL5947135 |
| 10.72 | EC50 | 0.019 | nM | CHEMBL5971655 |
| 10.72 | EC50 | 0.019 | nM | CHEMBL5840628 |
| 10.70 | EC50 | 0.02 | nM | CHEMBL5930370 |
| 10.70 | EC50 | 0.02 | nM | CHEMBL5876457 |
| 10.70 | EC50 | 0.02 | nM | CHEMBL5816213 |
| 10.68 | EC50 | 0.021 | nM | CHEMBL5817118 |
| 10.62 | EC50 | 0.024 | nM | CHEMBL5755111 |
| 10.62 | EC50 | 0.024 | nM | CHEMBL5858242 |
| 10.62 | EC50 | 0.024 | nM | CHEMBL5979599 |
| 10.60 | EC50 | 0.025 | nM | CHEMBL5811264 |
| 10.60 | EC50 | 0.025 | nM | CHEMBL5778806 |
| 10.59 | EC50 | 0.026 | nM | CHEMBL5878312 |
| 10.57 | EC50 | 0.027 | nM | CHEMBL5993382 |
| 10.57 | EC50 | 0.027 | nM | CHEMBL5850242 |
| 10.55 | EC50 | 0.028 | nM | CHEMBL5844639 |
| 10.55 | EC50 | 0.028 | nM | CHEMBL5840143 |
| 10.55 | EC50 | 0.028 | nM | CHEMBL6039670 |
| 10.55 | EC50 | 0.028 | nM | CHEMBL5919201 |
| 10.54 | EC50 | 0.029 | nM | CHEMBL5843772 |
| 10.52 | EC50 | 0.03 | nM | CHEMBL5882012 |
| 10.52 | EC50 | 0.03 | nM | CHEMBL6062016 |
| 10.49 | EC50 | 0.032 | nM | CHEMBL5844431 |
| 10.48 | EC50 | 0.033 | nM | CHEMBL5918071 |
| 10.47 | EC50 | 0.034 | nM | CHEMBL5935643 |
| 10.42 | EC50 | 0.038 | nM | CHEMBL5899256 |
PubChem BioAssay actives
1440 with measured affinity, of 1939 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 6-isoquinolin-4-yl-1-methyl-3,4-dihydroquinolin-2-one | 389805: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0001 | uM |
| Etomidate | 553066: Inhibition of human CYP11B2 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate | ic50 | 0.0001 | uM |
| 4-(6,7-difluoro-1-methylbenzimidazol-2-yl)isoquinoline | 1177651: Inhibition of human aldosterone synthase expressed in V79 MZ cells | ic50 | 0.0001 | uM |
| 5-chloro-2-[5-[2-(1-ethylpyrazole-4-carbonyl)-2,6-diazaspiro[3.3]heptan-6-yl]-3-pyridinyl]-3,3-dimethylisoindol-1-one | 2109202: Inhibition of human CYP11B2 stably expressed in G-402 cells | ic50 | 0.0002 | uM |
| 3-(methoxymethyl)-5-(6-methoxynaphthalen-2-yl)pyridine | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0002 | uM |
| 3-(1-methoxyethyl)-5-(6-methoxynaphthalen-2-yl)pyridine | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0002 | uM |
| 6-isoquinolin-4-yl-3,4-dihydro-1H-quinolin-2-one | 389805: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0002 | uM |
| 6-(5-methoxy-3-pyridinyl)-1-methyl-3,4-dihydroquinolin-2-one | 389805: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0002 | uM |
| Osilodrostat | 1154696: Inhibition of CYP11B2 (unknown origin) | ic50 | 0.0002 | uM |
| 6-isoquinolin-4-yl-1-azatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-11-one | 592041: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells assessed as conversion of [4-14C]-11-deoxycorticosterone substrate by HPTLC assay | ic50 | 0.0002 | uM |
| 7-isoquinolin-4-yl-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-2-one | 592041: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells assessed as conversion of [4-14C]-11-deoxycorticosterone substrate by HPTLC assay | ic50 | 0.0002 | uM |
| 1-cyclopropyl-2-(4,5-dimethyl-3-pyridinyl)-5,6-difluorobenzimidazole | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0002 | uM |
| 2-[5-(4-chloro-7-fluoroindazol-1-yl)-3-pyridinyl]propan-2-ol | 1474789: Inhibition of human CYP11B2-CLE9 expressed in Chinese hamster V79 cells using 11-deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition measured for 3 hrs by HTRF assay | ic50 | 0.0002 | uM |
| 2-fluoro-4-[5-(2-methyl-1,3-dioxolan-2-yl)-3-pyridinyl]benzonitrile | 1977386: Inhibition of human CYP11B2 stably transfected in mouse Y-1 cells using deoxycortisol or deoxycorticosterone as substrate incubated for 48 hrs by radioimmuno assay | ic50 | 0.0003 | uM |
| 2-[5-(4,7-difluoroindazol-1-yl)-3-pyridinyl]propan-2-ol | 1474789: Inhibition of human CYP11B2-CLE9 expressed in Chinese hamster V79 cells using 11-deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition measured for 3 hrs by HTRF assay | ic50 | 0.0003 | uM |
| 6-isoquinolin-4-yl-1,4-dihydro-3,1-benzoxazin-2-one | 1191378: Inhibition of CYP11B2 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 45 mins by HPLC analysis | ic50 | 0.0003 | uM |
| (1S)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxo-1,4-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol | 493924: Inhibition of human recombinant CYP11B2 by cell-based assay | ic50 | 0.0003 | uM |
| 2-[5-(1-cyclopropyl-5,6-difluorobenzimidazol-2-yl)-3-pyridinyl]propan-2-ol | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0003 | uM |
| [4-(4-fluorophenyl)sulfanylpyrimidin-5-yl]-(1-methylsulfonylpiperidin-4-yl)methanol | 1444794: Inhibition of human CYP11B2 expressed in HEK293A cells using deoxycorticosterone as substrate pretreated for 1 hr followed by substrate addition measured after 1 hr by HTRF assay | ic50 | 0.0004 | uM |
| 6-chloro-1-cyclopropyl-5-fluoro-2-pyridin-3-ylbenzimidazole | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0004 | uM |
| 1-cyclopropyl-5,6-difluoro-2-(5-methoxy-3-pyridinyl)benzimidazole | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0004 | uM |
| 3-(4-fluorophenyl)-4-[(5R)-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl]benzonitrile | 1059816: Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrate by cell-based assay | ic50 | 0.0004 | uM |
| 5-chloro-3,3-dimethyl-2-[5-[1-(1-methylpyrazole-4-carbonyl)azetidin-3-yl]oxy-3-pyridinyl]isoindol-1-one | 1658216: Inhibition of human CYP11B2 expressed in human renal leiomyoblastoma cells harboring FDXR/FDX using 1-deoxycorticosterone as substrate by HTRF assay | ic50 | 0.0005 | uM |
| 1-[5-(6-methoxynaphthalen-2-yl)-3-pyridinyl]ethanol | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0005 | uM |
| 4-(6-methoxy-3-methyl-3,4-dihydronaphthalen-2-yl)isoquinoline | 2109203: Inhibition of human CYP11B2 expressed in human NCI-H295 cells incubated for 48 hrs by radioimmuno assay | ic50 | 0.0005 | uM |
| 7-isoquinolin-4-yl-4H-1,4-benzoxazin-3-one | 1191378: Inhibition of CYP11B2 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 45 mins by HPLC analysis | ic50 | 0.0005 | uM |
| 1-cyclopropyl-5,6-difluoro-2-(5-fluoro-4-methyl-3-pyridinyl)benzimidazole | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0005 | uM |
| 2-phenyl-5-[(5-phenyl-3-pyridinyl)methyl]pyridine | 765521: Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate | ic50 | 0.0005 | uM |
| 3-cyclopropyl-6-fluoro-2-pyridin-3-ylbenzimidazole-5-carbonitrile | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0006 | uM |
| N-(4-fluorophenyl)-5-(1-methylsulfonylpiperidin-4-yl)sulfanylpyrimidin-4-amine | 2109497: Inhibition of human CYP11B2 expressed in HEK293-A cells harboring FDXR/FDX using deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr | ic50 | 0.0006 | uM |
| 4-(6-methoxynaphthalen-2-yl)isoquinoline | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0006 | uM |
| 6-(4-methyl-3-pyridinyl)naphthalene-2-carbonitrile | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0006 | uM |
| 6-(5-methoxy-3-pyridinyl)-1-azatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-11-one | 592041: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells assessed as conversion of [4-14C]-11-deoxycorticosterone substrate by HPTLC assay | ic50 | 0.0006 | uM |
| 1-cyclopropyl-5,6-difluoro-2-(4-methoxy-5-methyl-3-pyridinyl)benzimidazole | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0006 | uM |
| 4-(3-cyclopropyl-6-fluoroimidazo[1,2-a]pyridin-2-yl)isoquinoline | 1332279: Inhibition of human CYP11B2-CLE9 expressed in Chinese hamster V79 cells using 11-deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition measured after 3 hrs by HTRF assay | ic50 | 0.0006 | uM |
| 1-(5-isoquinolin-4-ylindol-1-yl)ethanone | 1154700: Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate | ic50 | 0.0006 | uM |
| 2,2,2-trifluoro-1-[4-(4-fluoroanilino)pyrimidin-5-yl]-1-(1-methylsulfonylpiperidin-4-yl)ethanol | 1444794: Inhibition of human CYP11B2 expressed in HEK293A cells using deoxycorticosterone as substrate pretreated for 1 hr followed by substrate addition measured after 1 hr by HTRF assay | ic50 | 0.0007 | uM |
| 6-[5-(2-fluorophenyl)-3-pyridinyl]-1-azatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-11-one | 592041: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells assessed as conversion of [4-14C]-11-deoxycorticosterone substrate by HPTLC assay | ic50 | 0.0007 | uM |
| 1-(5-isoquinolin-4-yl-2,3-dihydroindol-1-yl)ethanone | 1154700: Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate | ic50 | 0.0007 | uM |
| 4-[6-(diethylamino)pyrazin-2-yl]-2-fluorobenzonitrile | 1977386: Inhibition of human CYP11B2 stably transfected in mouse Y-1 cells using deoxycortisol or deoxycorticosterone as substrate incubated for 48 hrs by radioimmuno assay | ic50 | 0.0008 | uM |
| N-(4-fluorophenyl)-5-(1-methylsulfonylpiperidin-4-yl)sulfonylpyrimidin-4-amine | 2109497: Inhibition of human CYP11B2 expressed in HEK293-A cells harboring FDXR/FDX using deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr | ic50 | 0.0008 | uM |
| methyl 5-(6-methoxynaphthalen-2-yl)pyridine-3-carboxylate | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0008 | uM |
| 3-(6-methoxynaphthalen-2-yl)-4-methylpyridine | 362124: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | ic50 | 0.0008 | uM |
| 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(propan-2-yloxymethyl)-1,4-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide | 493924: Inhibition of human recombinant CYP11B2 by cell-based assay | ic50 | 0.0008 | uM |
| 6-chloro-1-cyclopropyl-5-fluoro-2-(5-fluoro-3-pyridinyl)benzimidazole | 1229390: Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay | ic50 | 0.0008 | uM |
| 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile | 1154700: Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate | ic50 | 0.0008 | uM |
| 4-[6-(dimethylamino)pyrazin-2-yl]-2-fluorobenzonitrile | 1977386: Inhibition of human CYP11B2 stably transfected in mouse Y-1 cells using deoxycortisol or deoxycorticosterone as substrate incubated for 48 hrs by radioimmuno assay | ic50 | 0.0009 | uM |
| 2-fluoro-4-[5-(4-methyl-1,3-dioxolan-2-yl)-3-pyridinyl]benzonitrile | 1977386: Inhibition of human CYP11B2 stably transfected in mouse Y-1 cells using deoxycortisol or deoxycorticosterone as substrate incubated for 48 hrs by radioimmuno assay | ic50 | 0.0009 | uM |
| N-(4-fluorophenyl)-5-(4-methylsulfonylpiperazin-1-yl)sulfonylpyrimidin-4-amine | 2109497: Inhibition of human CYP11B2 expressed in HEK293-A cells harboring FDXR/FDX using deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr | ic50 | 0.0009 | uM |
| 7-(5-methoxy-3-pyridinyl)-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-2-one | 592041: Inhibition of human CYP11B2 expressed in hamster V79 MZh cells assessed as conversion of [4-14C]-11-deoxycorticosterone substrate by HPTLC assay | ic50 | 0.0009 | uM |
CTD chemical–gene interactions
109 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Colforsin | decreases expression, increases expression, decreases reaction, increases reaction, affects cotreatment (+1 more) | 10 |
| 3,4,5,3’,4’-pentachlorobiphenyl | increases activity, increases expression, increases reaction, affects cotreatment | 6 |
| Aldosterone | increases chemical synthesis, increases hydroxylation, affects chemical synthesis | 5 |
| torcetrapib | increases expression, decreases reaction | 4 |
| Fadrozole | decreases activity | 4 |
| Flame Retardants | increases expression, decreases expression | 3 |
| Ketoconazole | affects binding, decreases activity, increases expression, increases reaction | 3 |
| tributyltin | affects cotreatment, increases expression | 2 |
| 2,4,5,2’,4’,5’-hexachlorobiphenyl | increases expression, affects cotreatment | 2 |
| perfluorooctane sulfonic acid | increases expression, affects cotreatment | 2 |
| 2,2’,4,4’-tetrabromodiphenyl ether | increases expression, affects cotreatment | 2 |
| Benzo(a)pyrene | affects methylation, increases expression | 2 |
| Corticosterone | affects metabolic processing, increases chemical synthesis, increases hydroxylation | 2 |
| Cortodoxone | affects metabolic processing, increases metabolic processing | 2 |
| Desoxycorticosterone | increases chemical synthesis, affects metabolic processing, increases hydroxylation | 2 |
| Potassium | increases expression, decreases reaction | 2 |
| Valproic Acid | increases expression, increases methylation | 2 |
| 8-Bromo Cyclic Adenosine Monophosphate | increases expression | 2 |
| Halogenated Diphenyl Ethers | decreases expression, increases expression | 2 |
| fluorene-9-bisphenol | affects reaction, increases expression, decreases expression | 1 |
| triptolide | decreases expression, affects cotreatment | 1 |
| perflubron | increases expression | 1 |
| 2,4,6-tribromophenol | decreases expression | 1 |
| methylmercuric chloride | increases expression, affects cotreatment | 1 |
| alternariol | increases expression | 1 |
| naringin | decreases reaction, increases expression | 1 |
| bisphenol A | decreases expression | 1 |
| deoxynivalenol | increases expression | 1 |
| 4,4’-bisphenol F | decreases expression | 1 |
| 2,4,5,2’,5’-pentachlorobiphenyl | increases expression | 1 |
ChEMBL screening assays
147 unique, capped per target: 135 binding, 12 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1002226 | Binding | Inhibition of human CYP11B2 expressed in hamster V79 MZh cells | Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity. — J Med Chem |
| CHEMBL2433420 | ADMET | Inhibition of human CYP11B2 | Emerging technologies for metabolite generation and structural diversification. — Bioorg Med Chem Lett |
Cellosaurus cell lines
1 cell lines: 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_4710 | V79MZh11B2 | Spontaneously immortalized cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Associated diseases: corticosterone methyloxidase type 1 deficiency, corticosterone methyloxidase type 2 deficiency, familial hypoaldosteronism, familial hyperreninemic hypoaldosteronism type 2
- Targeted by drugs: Baxdrostat, Lorundrostat, Metyrapone, Osilodrostat
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): corticosterone methyloxidase type 1 deficiency, corticosterone methyloxidase type 2 deficiency, early-onset familial hypoaldosteronism, familial hyperreninemic hypoaldosteronism type 2, familial hypoaldosteronism, glucocorticoid-remediable aldosteronism